The androgen insensitivity syndrome is a heterogeneous disorder with a wide spectrum of phenotypic abnormalities, ranging from complete female to ambiguous forms that more closely resembles males. Mutations of the androgen receptor gene are responsible for a variable degree of impaired androgen action. The complete androgen insensitivity syndrome is characterized by normal female external appearance in spite of the normal male karyotype 46XY with testes and normal testosterone production and metabolism. This is transmitted by X-linked recessive manner. Wolffian duct does not develop. However, m llerian development does not occur in presence of antim llerian hormone activity. Recently we experienced a case of complete androgen insenditirity syndrome. We reported a case with concerned literatures.
Androgen-Insensitivity Syndrome* ; Female ; Humans ; Karyotype ; Male ; Metabolism ; Receptors, Androgen ; Testis ; Testosterone ; Wolffian Ducts

OBJECTIVESTo study the coexistence of androgen receptor(AR) and GnRH receptor(GnRHR), and further identify that submaxillary is a target organ of androgen and GnRH in SD Rat.

METHODSSequential deparaffinized sections of SD rat submaxillary were immunostained with SABC method. The first antibodies were rabbit anti-rat GnRH idiotypic antibodies and mouse anti-rat androgen receptor antibodies.

RESULTSAR immunoreactive cells were found in glandular epithelial cells of serous acinus and epithelial cells in all gland ducts. While the distribution of GnRHR coincides with that of AR. The immunoreactive substances were distributed in cytoplasm of all positive cells with negative nuclei.

CONCLUSIONSThe results showed that AR existed in submaxillary and was widely distributed in glandular epithelial cells with distributive pattern similar to those of GnRHR. It suggests that submaxillary is a target organ of androgen, responsible for modulating biological function of submaxillary.

Animals ; Immunohistochemistry ; Male ; Rats ; Rats, Sprague-Dawley ; Receptors, Androgen ; metabolism ; Receptors, LHRH ; metabolism ; Submandibular Gland ; metabolism

Androgens control a broad range of physiological functions. The androgen receptor (AR), a steroid receptor that mediates the diverse biological actions of androgens, is a ligand inducible transcription factor. Abnormalities in the androgen signaling system result in many disturbances ranging from changes in gender determination and sexual development to psychiatric and emotional disorders. Androgen replacement therapy can improve many clinical conditions including hypogonadism and osteoporosis, but is limited by the lack of efficacious and safe therapeutic agents with easy delivery options. Recent progress in the area of gene regulation by steroid receptors and by selective receptor modulators provides an opportunity to examine if selective androgen receptor modulators (SARMs) could address some of the problems associated with current androgen therapy. Since the composition of the transcriptional initiation complex recruited by liganded AR determines the specificity of gene regulation, synthetic ligands aimed at initiating transcription of tissue and promoter specific genes offers hope for developing better androgen therapy. Establishment of assays that predict synthetic ligand activity is critical for SARM development. Advancement in high throughput compound screening and gene fingerprinting technologies, such as microarrays and proteomics, will facilitate and accelerate identification of effective SARMs.
Androgen Antagonists ; pharmacology ; Androgen Receptor Antagonists ; Androgens ; chemistry ; metabolism ; Chlormadinone Acetate ; analogs & derivatives ; pharmacology ; Humans ; Male ; Receptors, Androgen ; physiology ; Receptors, Cytoplasmic and Nuclear ; physiology ; Testosterone Congeners ; pharmacology

OBJECTIVESTo investigate the androgen receptor (AR) isoforms expression in human benign and malignant prostatic tissues and LNCaP cells.

METHODSUsing high resolution isoelectric focusing (IEF), the different expression of AR isoforms were demosntrated in human benign and malignant prostatic tissues and LNCaP cells.

RESULTSData were obtained from 41 AR-positive BPH, three prostatic cancer specimens, and LNCaP cells. From these materials, three types of AR isoforms were detected with pI values at 6.5, 6.0 and 5.3. In the case of BPH tissues, 15 (36.5%) specimens expressed all the three types of isoforms at pI 6.5, 6.0 and 5.3, and 10 (24.4%) samples contained isoforms at pI 6.5 and 5.3, five (12.2%) samples indicated isoforms at pI 6.5 and 6.0, four (9.8%) showed the isoforms at pI 6.0 and 5.3. Of all the 41 specimens, two (4.9%) and two (4.9%) as well as three (7.3%) denoted the isoforme at pI 6.5, 6.0 and 5.3 respectively. As for three prostatic cancer specimens, one sample showed all the three types of AR isoforms at pI 6.5, 6.0, 5.3, but another specimen expressed at pI 6.5 and 6.0, and only one failed to indicate any types of isoforms. LNCaP cells expressed all three types of AR isoforms at pI 6.5, 6.0 and 5.3. Binding of 3H-dihydrotestosterone to these three types of isoforms was inhibited by the addition of 100-fold excess of DHT and testosterone. No effect of progesterone, oestradiol and diethylstilboestrol on tritiated hormone binding was observed.

CONCLUSIONSThe expression of AR isoforms is different among various patients and different between BPH and LNCaP cells, though no clear explanation could be induced for this. These results suggest the possibility of explaining effective hormonal therapy to prostatic disease in the future.

Humans ; Male ; Prostate ; metabolism ; Protein Isoforms ; metabolism ; Receptors, Androgen ; metabolism ; Tumor Cells, Cultured

Prostate cancer (PCa) is one of the most common malignancies in the urinary system of males. A growing number of studies have shown that microRNAs, as small ribonucleic acid molecules and a class of non-coding small RNAs, are closely related with PCa and a variety of microRNAs are abnormally expressed in it. This article focuses on the roles of microRNAs in the occurrence and progression of PCa, with a description of differentially expressed microRNAs in PCa and an analysis of their association with its prognosis as well as their correlation with chemotherapy, androgen receptors, and metastasis of PCa.
Disease Progression ; Humans ; Male ; MicroRNAs ; metabolism ; Prognosis ; Prostatic Neoplasms ; chemistry ; genetics ; metabolism ; Receptors, Androgen ; metabolism

Ubiquitin is a small molecule protein consisting of 76 amino acids,widely found in eukaryotic cells. The process by which ubiquitin binding to a specific protein is called ubiquitination. Deubiquitination is the reversed process of ubiquitination. Ubiquitination stimulates downstream signal,including complex assembly,protein conformation and activity changes,proteolysis,autophagy,guilt,chromatin remodeling,and DNA repair. More than 80% of eukaryotic protein degradation is mediated by the ubiquitination system,and ubiquitin-dependent proteolysis is an extremely complex process involving many biomolecular processes. By regulating protein homeostasis,ubiquitination can also regulate a variety of biological processes including cell cycle,cell proliferation,and apoptosis,which are closely related to tumorigenesis and progression. Many abnormalities of androgen receptor (AR) including AR gene amplification,mutation,shear mutation,and AR activity enhancement are closely related to prostate cancer progression. In particular,prostate cancer progression is regulated by the ubiquitination/deubiquitination processes. This article summarizes the recent research advances in the roles of ubiquitination/deubiquitination in AR abnormalities and prostate cancer.
Cell Line, Tumor ; Humans ; Male ; Prostatic Neoplasms ; metabolism ; pathology ; Proteolysis ; Receptors, Androgen ; metabolism ; Ubiquitination

Androgen receptor(AR) plays an important role in modulating the effects of androgen on target cells. It is well known that AR is mainly existed in testis. This paper reviewed the distribution of AR and its mRNA in prostate, epididymis, skin of penis, and some other tissues in non-genital system and tumors, such as the skin of scalp, hippocampus, fat, gastric cancer, cancer of larynx, and so on. Besides, this paper also reviewed the detection methods to AR, and further investigated the function of androgen.
Androgens ; metabolism ; Hippocampus ; metabolism ; Humans ; Male ; Penis ; metabolism ; Prostate ; metabolism ; Receptors, Androgen ; metabolism ; Testis ; metabolism ; Tissue Distribution ; Tumor Cells, Cultured

Apoptosis ; Breast Neoplasms ; metabolism ; pathology ; Female ; Humans ; MicroRNAs ; metabolism ; physiology ; Receptor, ErbB-2 ; metabolism ; Receptors, Androgen ; metabolism ; Receptors, Estrogen ; metabolism ; Receptors, Progesterone ; metabolism ; Signal Transduction

Most prostate cancers initially respond to androgen deprivation therapy (ADT). With the long-term application of ADT, localized prostate cancer will progress to castration-resistant prostate cancer (CRPC), metastatic CRPC (mCRPC), and neuroendocrine prostate cancer (NEPC), and the transcriptional network shifted. Forkhead box protein A1 (FOXA1) may play a key role in this process through multiple mechanisms. To better understand the role of FOXA1 in prostate cancer, we review the interplay among FOXA1-targeted genes, modulators of FOXA1, and FOXA1 with a particular emphasis on androgen receptor (AR) function. Furthermore, we discuss the distinct role of FOXA1 mutations in prostate cancer and clinical significance of FOXA1. We summarize possible regulation pathways of FOXA1 in different stages of prostate cancer. We focus on links between FOXA1 and AR, which may play different roles in various types of prostate cancer. Finally, we discuss FOXA1 mutation and its clinical significance in prostate cancer. FOXA1 regulates the development of prostate cancer through various pathways, and it could be a biomarker for mCRPC and NEPC. Future efforts need to focus on mechanisms underlying mutation of FOXA1 in advanced prostate cancer. We believe that FOXA1 would be a prognostic marker and therapeutic target in prostate cancer.
Humans ; Male ; Androgen Antagonists/therapeutic use* ; Androgens/metabolism* ; Hepatocyte Nuclear Factor 3-alpha/metabolism* ; Mutation ; Prostatic Neoplasms, Castration-Resistant/drug therapy* ; Receptors, Androgen/metabolism*

OBJECTIVETo investigate the expression of androgen receptor (AR) isoforms in normal human prostate.

METHODSFourteen normal prostatic specimens from donors, aged 25 on average (21-28 yr), were analyzed by high resolution isoelectric focusing (IEF). The expression of AR isoforms was demonstrated in all 14 normal human prostatic tissues.

RESULTSFour types of AR isoforms were detected with isoelectric point value at 6.5, 6.0, 5.8 and 5.3 in 14 prostatic specimens. Binding of 3H-dihydrotestosterone (DHT) to these four AR isoforms was inhibited by the addition of 100-fold excess of DHT and testosterone. No effect of progesterone, estradiol and diethylstilbestrol on tritiated hormone binding was observed.

CONCLUSIONSThere are four AR isoforms in normal human prostate. The expression of AR isoforms is different from one another.

Adult ; Humans ; Isoelectric Focusing ; Isoelectric Point ; Male ; Prostate ; metabolism ; Protein Isoforms ; biosynthesis ; Receptors, Androgen ; biosynthesis